CN111757735B - 用于治疗激酶依赖性病症的化合物 - Google Patents

用于治疗激酶依赖性病症的化合物 Download PDF

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CN111757735B
CN111757735B CN201980015066.9A CN201980015066A CN111757735B CN 111757735 B CN111757735 B CN 111757735B CN 201980015066 A CN201980015066 A CN 201980015066A CN 111757735 B CN111757735 B CN 111757735B
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alkyl
alkylene
optionally substituted
cell
cancer
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CN111757735A (zh
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L·C·班宁
M·别伊
蒋发明
曹健雲
王勇
许维
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Exelixis Inc
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Exelixis Inc
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Priority to CN202311157242.7A priority Critical patent/CN117402114A/zh
Priority to CN202311131715.6A priority patent/CN117603138A/zh
Priority to CN202311123887.9A priority patent/CN117820226A/zh
Priority to CN202311144729.1A priority patent/CN117624045A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
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    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/60—Quinoline or hydrogenated quinoline ring systems
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
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  • Chemical & Material Sciences (AREA)
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  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Biochemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Peptides Or Proteins (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Quinoline Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201980015066.9A 2018-01-26 2019-01-25 用于治疗激酶依赖性病症的化合物 Active CN111757735B (zh)

Priority Applications (4)

Application Number Priority Date Filing Date Title
CN202311157242.7A CN117402114A (zh) 2018-01-26 2019-01-25 用于治疗激酶依赖性病症的化合物
CN202311131715.6A CN117603138A (zh) 2018-01-26 2019-01-25 用于治疗激酶依赖性病症的化合物
CN202311123887.9A CN117820226A (zh) 2018-01-26 2019-01-25 用于治疗激酶依赖性病症的化合物
CN202311144729.1A CN117624045A (zh) 2018-01-26 2019-01-25 用于治疗激酶依赖性病症的化合物

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862622702P 2018-01-26 2018-01-26
US62/622,702 2018-01-26
US201862758321P 2018-11-09 2018-11-09
US62/758,321 2018-11-09
PCT/US2019/015297 WO2019148044A1 (fr) 2018-01-26 2019-01-25 Composés destinés au traitement de troubles dépendant de la kinase

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CN202311157242.7A Division CN117402114A (zh) 2018-01-26 2019-01-25 用于治疗激酶依赖性病症的化合物
CN202311144729.1A Division CN117624045A (zh) 2018-01-26 2019-01-25 用于治疗激酶依赖性病症的化合物
CN202311123887.9A Division CN117820226A (zh) 2018-01-26 2019-01-25 用于治疗激酶依赖性病症的化合物
CN202311131715.6A Division CN117603138A (zh) 2018-01-26 2019-01-25 用于治疗激酶依赖性病症的化合物

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CN111757735A CN111757735A (zh) 2020-10-09
CN111757735B true CN111757735B (zh) 2023-09-22

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CN201980015066.9A Active CN111757735B (zh) 2018-01-26 2019-01-25 用于治疗激酶依赖性病症的化合物
CN202311157242.7A Pending CN117402114A (zh) 2018-01-26 2019-01-25 用于治疗激酶依赖性病症的化合物
CN202311144729.1A Pending CN117624045A (zh) 2018-01-26 2019-01-25 用于治疗激酶依赖性病症的化合物
CN202311131715.6A Pending CN117603138A (zh) 2018-01-26 2019-01-25 用于治疗激酶依赖性病症的化合物
CN202311123887.9A Pending CN117820226A (zh) 2018-01-26 2019-01-25 用于治疗激酶依赖性病症的化合物

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CN202311157242.7A Pending CN117402114A (zh) 2018-01-26 2019-01-25 用于治疗激酶依赖性病症的化合物
CN202311144729.1A Pending CN117624045A (zh) 2018-01-26 2019-01-25 用于治疗激酶依赖性病症的化合物
CN202311131715.6A Pending CN117603138A (zh) 2018-01-26 2019-01-25 用于治疗激酶依赖性病症的化合物
CN202311123887.9A Pending CN117820226A (zh) 2018-01-26 2019-01-25 用于治疗激酶依赖性病症的化合物

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US (2) US11542259B2 (fr)
EP (2) EP4647127A3 (fr)
JP (3) JP7321165B2 (fr)
KR (2) KR102721118B1 (fr)
CN (5) CN111757735B (fr)
AU (2) AU2019212801B2 (fr)
BR (1) BR112020015201A2 (fr)
CA (1) CA3088200A1 (fr)
CL (2) CL2020001931A1 (fr)
CO (1) CO2020010465A2 (fr)
CR (2) CR20230287A (fr)
DK (1) DK3743070T3 (fr)
ES (1) ES3048989T3 (fr)
FI (1) FI3743070T3 (fr)
GE (2) GEAP202415420A (fr)
HR (1) HRP20251184T1 (fr)
HU (1) HUE073371T2 (fr)
IL (3) IL321138A (fr)
LT (1) LT3743070T (fr)
MA (1) MA51673B1 (fr)
MD (1) MD3743070T2 (fr)
MX (2) MX2020007765A (fr)
MY (1) MY210421A (fr)
PE (2) PE20242219A1 (fr)
PH (1) PH12020551208A1 (fr)
PL (1) PL3743070T3 (fr)
PT (1) PT3743070T (fr)
RS (1) RS67317B1 (fr)
SA (1) SA520412500B1 (fr)
SG (1) SG11202006921PA (fr)
SI (1) SI3743070T1 (fr)
SM (1) SMT202500395T1 (fr)
UA (1) UA128476C2 (fr)
WO (1) WO2019148044A1 (fr)

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CN111936487B (zh) 2018-01-26 2024-07-09 埃克塞里艾克西斯公司 用于治疗激酶依赖性病症的化合物
GEAP202415420A (en) * 2018-01-26 2024-12-25 Exelixis Inc Compounds for the treatment of kinase-dependent disorders
AU2019375983A1 (en) 2018-11-09 2021-06-10 Vivace Therapeutics, Inc. Bicyclic compounds
EP4631505A3 (fr) * 2018-12-13 2025-12-10 Exelixis, Inc. Formes cristallines et formes salines d'un inhibiteur de kinase
CA3126721A1 (fr) * 2019-01-25 2020-07-30 Exelixis, Inc. Composes pour le traitement de troubles dependant de la kinase
CN109761899B (zh) * 2019-02-14 2022-11-15 广州六顺生物科技股份有限公司 喹啉衍生物、其药学上可接受的盐或其溶剂合物、其应用、药物及药物组合物
IL287222B2 (en) 2019-04-16 2025-04-01 Vivace Therapeutics Inc Bicyclic compounds
SG11202111978VA (en) * 2019-06-03 2021-11-29 Exelixis Inc Crystalline salt forms of a kinase inhibitor
AR119069A1 (es) * 2019-06-04 2021-11-24 Exelixis Inc Compuestos para el tratamiento de trastornos dependientes de quinasas
CN110845406B (zh) * 2019-12-04 2021-07-20 广州安岩仁医药科技有限公司 喹啉类化合物的制备方法
US12545654B2 (en) 2020-02-10 2026-02-10 Stemsynergy Therapeutics, Inc. MYC inhibitors and uses thereof
PE20230110A1 (es) * 2020-04-30 2023-01-25 Exelixis Inc Procesos para la preparacion de un inhibidor de cinasa
BR112023001792A2 (pt) * 2020-07-31 2023-04-11 Exelixis Inc Combinações para o tratamento de câncer
MX2023005273A (es) 2020-11-05 2023-05-23 Exelixis Inc Composiciones farmaceuticas de un inhibidor de cinasa.
WO2022161447A1 (fr) * 2021-02-01 2022-08-04 江苏恒瑞医药股份有限公司 Composé dicarboxamide, son procédé de préparation et son utilisation pharmaceutique
CA3207513A1 (fr) * 2021-02-17 2022-08-25 Kristin Patterson Solides cristallins d'inhibiteur de mek n-((r)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-benzamide et utilisations associees
CN113582924A (zh) * 2021-09-09 2021-11-02 四川国康药业有限公司 一种多靶点酪氨酸激酶抑制剂及其制备方法和用途
AR127561A1 (es) * 2021-11-03 2024-02-07 Exelixis Inc Compuestos para el tratamiento de trastornos dependientes de cinasas
JP2025500436A (ja) 2021-12-22 2025-01-09 エグゼリクシス， インコーポレイテッド キナーゼ阻害剤の結晶性形態及び塩形態
CN114573553B (zh) * 2022-01-27 2023-11-10 广州六顺生物科技有限公司 杂芳环类衍生物及其制备方法和应用
CN116655626B (zh) * 2023-05-24 2025-03-11 遵义医科大学 一种含咪唑并[l，2-a]吡啶骨架的环丙二酰胺化合物及其制备方法和用途
CN116751161A (zh) * 2023-06-28 2023-09-15 中国人民解放军军事科学院军事医学研究院 喹啉类化合物及其制备方法、药物组合物及医药用途
WO2025253311A1 (fr) 2024-06-04 2025-12-11 Hetero Labs Limited Composés 1,2-dicarboxamide utilisés en tant qu'inhibiteurs de kinase
WO2026074526A1 (fr) 2024-10-04 2026-04-09 Hetero Labs Limited Composés 1,2-dicarboxamide utilisés en tant qu'inhibiteurs de kinase

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CN106400155A (zh) * 2016-08-31 2017-02-15 飞佛特种纺织品（宁波）有限公司 一种防老化阳光面料
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